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Styryl compound modified by azo-containing heterocyclic and use thereof

A styryl, compound technology, applied in non-active ingredients medical preparations, organic chemistry, drug combinations, etc., can solve problems such as unclear, neurofibrillary tangles, and inability to prevent the occurrence and development of diseases

Inactive Publication Date: 2009-10-21
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For many years, the main drug for clinical treatment of this disease is cholinesterase inhibitor, which acts on the cholinergic nervous system and has a relieving effect on the disease, but it cannot prevent the occurrence and development of the disease
At present, the pathogenesis of Alzheimer's disease is not very clear, but it is generally believed that the key cause of the disease is the aggregate (SP) formed by misfolding of excess β-amyloid peptide (Aβ). main component) damages cell membranes, synapses and axons, and causes neurofibrillary tangles

Method used

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  • Styryl compound modified by azo-containing heterocyclic and use thereof
  • Styryl compound modified by azo-containing heterocyclic and use thereof
  • Styryl compound modified by azo-containing heterocyclic and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1, the preparation of styryl compound

[0036] Synthesizing the styrene-based compound of the present invention comprises the following steps:

[0037] a. Synthesize the monomer [4,7,10-tri-tert-butoxycarbonyl-1,4,7,10-tetraazacyclododecyl-1-yl] acetic acid containing Cyclen, the method is: with Cyclen (purchased From Acros Company of the United States as a raw material, first react with Boc2O (di-tert-butyl dicarbonate, purchased from Shanghai Gil Biochemical Company) to obtain 1,4,7-tri-tert-butoxycarbonyl-1,4,7,10-tetraaza 3Boc-Cyclen (see Eiichi Kimura, Shin Aoki, Tohru Koike, and Motoo Shiro, A Tris(ZnII-1, 4, 7, 10-tetraazacyclododecane) Complex as a New Receptor for Phosphate Dianions in Aqueous Solution, Journal of American Chemical Society, 1997, Vol 119, 3068-3076), and then react the product with ethyl bromoacetate (see Joong Won Jeon, SangJun Son, Chang Eun Yoo, In Seok Hong, Jung Bae Song, and Junghun Suh, Protein-Cleaving Catalyst Selective fo...

Embodiment 2

[0043] Embodiment 2, the preparation of styryl compound

[0044] Synthetic styrene-based compound (formula VII) of the present invention comprises the following steps:

[0045] a. Mix benzoic acid (purchased from Sigma, USA) with Cyclen-containing monomer [4,7,10-tri-tert-butoxycarbonyl-1,4,7,10-tetraazacyclododecyl-1-yl ] Coupling with acetic acid, the connection condition is in the presence of coupling agent EDC (purchased from Shanghai Yanchang Biochemical Company), HOBt (purchased from Shanghai Jill Biochemical Company) and catalytic DMAP (mixing ratio: 4 times the monomer containing Cyclen, 1 times The amount of benzoic acid, 4 times the amount of coupling agent EDC and 4 times the amount of HOBt) were reacted at room temperature for 15 hours to obtain the target product.

[0046] c. The crude product obtained after the reaction of step b is separated with a silica gel column (column separation conditions are: ethyl acetate: petroleum ether (1:4)), and the resulting prod...

Embodiment 3

[0050] Embodiment 3, the preparation of styryl compound

[0051] Synthetic styrene-based compound of the present invention (molecular formula sees formula VIII), comprises the following steps:

[0052] a. Preparation of Trpn-containing monomer [3(3', 3"-di-tert-butoxycarbonyl-3', 3"-diamino)aminopropylamino]acetic acid: the synthesis method is: Trpn (purchased from the United States Acros Company) as a raw material, first react with Boc2O (di-tert-butyl dicarbonate, purchased from Shanghai Gil Biochemical Company) to obtain 3', 3"-di-tert-butoxycarbonyl-3,3', 3"-triaminopropyl Amine (2Boc-Trpn) (see Eiichi Kimura, Shin Aoki, Tohru Koike, and Motoo Shiro, ATris (ZnII-1, 4, 7, 10-tetraazacyclododecane) Complex as a New Receptor for Phosphate Dianions in Aqueous Solution, Journal of American Chemical Society, 1997, Vol 119, 3068-3076), and then react the product with ethyl bromoacetate (see Joong Won Jeon, Sang Jun Son, Chang Eun Yoo, In Seok Hong, Jung Bae Song, and Junghun Suh...

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PUM

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Abstract

This invention relates to an azacyclo-modified styrene compounds and its applications. Its purpose is to provide an azacyclo-modified styrene compounds, and its applications in the preparation of Alzheimer's disease, Parkinson's disease and other degenerative nervous system disease or type two diabetes prevention and therapeutic drug. Studies show that the invention can inhibit aggregation of A beta, also can make the A beta aggregate depolymerizate, and will eventually hydrolysis and eliminate A beta protein, inhibited and removal of A beta toxicity, in the field of medicine has broad application prospects.

Description

technical field [0001] The present invention relates to a styryl compound and its application, in particular to a styryl compound modified with a nitrogen-containing heterocycle and its use in the preparation, treatment and prevention of Alzheimer's disease, Parkinson's disease, type 2 diabetes and other nervous system Applications in Degenerative Disease Medicine. Background technique [0002] Neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease and type 2 diabetes are protein conformation diseases. Among them, Alzheimer's disease (AD), also known as Alzheimer's disease, is a degenerative disease of the central nervous system, clinically manifested as cognitive impairment, memory loss, and eventually loss of thinking ability, movement disorders, and life. Can not take care of themselves. The pathological features are mainly senile plaque (SP), neurofibrillary tangles (neurofibrillary tangles, NFT) and selective loss of neurons and synapses. As t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D225/02C07C229/16C07C237/06A61K47/48A61K31/19A61K31/665A61K31/216A61P25/28A61P25/16A61P3/10A61K47/54
Inventor 李艳梅吴为辉雷鹏苏小阳胡笳
Owner TSINGHUA UNIV
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